Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond

Author(s): Wei-Yao Wu, Sheng-Li Cao, Bei-Bei Mao, Ji Liao, Zhong-Feng Li, Hao-Bin Song, Xingzhi Xu.

Abstract:

A novel series of hybrids of indolin-2-one and quinazolin-4(3H)-one linked via an imine bond were synthesized and tested for their inhibitory activity against the proliferation of a panel of five human cancer cell lines. We found that compound 5c bearing 5-bromo substituent at the indolin-2-one ring exhibited weak cytotoxic activity with percentages of inhibition ranging from 27% to 49% at 20 μM, while its counterpart 7c having 4-methoxybenzyl group at the N1-position of indolin-2-one ring was more active with percentages of inhibition in range of 32-63%. These results indicate that the presence of a bromo substituent at the 5-position and a 4-methoxybenzyl group at the N1-position of indolin-2-one ring is important for the cytotoxic activity.

Keywords: Antitproliferative activity, Hybrid, Indolin-2-one, Quinazolin-4(3H)-one, Synthesis, gastrointestinal stromal tumor, Nolatrexed, 2-Methylquinazolin, nitroquinazolin, MTT Assay

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Article Details

VOLUME: 10
ISSUE: 1
Year: 2013
Page: [61 - 66]
Pages: 6
DOI: 10.2174/1570180811309010061